Recent Advances in Anti-Influenza Agents with Neuraminidase as Target

Abstract

Neuraminidase (NA) is the major surface glycoprotein of the influenza virus. It has been considered a suitable target for designing agents against influenza viruses. Rational drug design of NA inhibitors is now in the clinic and is effective for the treatment of influenza. Recently, research of structure-based NA inhibitors is becoming an interesting field, leading to a breakthrough in the control of influenza. Here we review a series of neuraminidase inhibitors and the recent progress in this field.

Combining docking, scoring and molecular field analyses to probe influenza neuraminidase–ligand interactions

“…All binding regions were implicated in substrate recognition, however, Asp151, Glu277 and Tyr406 are believed to play a critical role in the catalytic activity of NA [89,90]. Table 1).…”

Design, synthesis, and biological activity of thiazole derivatives as novel influenza neuraminidase inhibitors

“…All binding regions were implicated in substrate recognition; however, Asp 151, Glu 277, and Tyr 406 are believed to play a critical role in the catalytic activity of NA. (20,21) According to the studies on NA active site and SAR of published NA inhibitors, inhibition of the NA is mainly determined by the relative positions of the four substituents of the central ring. (22) For example, in oseltamivir, the four substituents are carboxyl ethyl ester, amino, acetamino, and alkyl.…”

Potential Targets and Their Relevant Inhibitors in Anti-influenza Fields

“…As a potent and long-acting NAI, dimeric zanamivir (41) could provide effective treatment and prophylaxis for influenza virus infections at a once-weekly dosing regimen [191,192]. Recent lessons from the discovery and development of NAIs have been reviewed in several papers elsewhere [20,[193][194][195][196]. influenza A virus NA could be divided into two distinct families: group 1 (N1, N4, N5, and N8 subtypes) and group 2 (N2, N3, N6, N7, and N9 subtypes).…”